title: Microemulsion for simultaneous transdermal delivery of benzocaine and indomethacin: in vitro and in vivo evaluation.
abstract: This study investigated simultaneous transdermal delivery of indomethacin and benzocaine from microemulsion. Eucalyptus oil based microemulsion was used with Tween 80 and ethanol being employed as surfactant and cosurfactant, respectively. A microemulsion formulation comprising eucalyptus oil, polyoxyethylene sorbitan momooleate (Tween 80), ethanol and water (20:30:30:20) was selected. Indomethacin (1% w/w) and benzocaine (20% w/w) were incorporated separately or combined into this formulation before in vitro and in vivo evaluation. Application of indomethacin microemulsion enhanced the transdermal flux and reduced the lag time compared to saturated aqueous control. The same trend was evident for benzocaine microemulsion. Simultaneous application of the two drugs in microemulsion provided similar enhancement pattern. The in vivo evaluation employed the pinprick method and revealed rapid anesthesia after application of benzocaine microemulsion with the onset being 10 min and the action lasting for 50 min. For indomethacin microemulsion, the analgesic effect was recorded after 34.5 min and lasted for 70.5 min. Simultaneous application of benzocaine and indomethacin provided synergistic effect. The onset of action was achieved after 10 min and lasted for 95 min. The study highlighted the potential of microemulsion formulation in simultaneous transdermal delivery of two drugs.
authors.affiliation: Department of Pharmaceutical Technology, College of Pharmacy, University of Tanta , Tanta , Egypt.
authors.forename: Gamal M
authors.initials: GM
authors.lastname: El Maghraby
authors.forename: Mona F
authors.initials: MF
authors.lastname: Arafa
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Osman
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D001566:Benzocaine / Q000008:administration & dosage* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage* / Q000378:metabolism; D006801:Humans; D007213:Indomethacin / Q000008:administration & dosage* / Q000378:metabolism; D009924:Organ Culture Techniques; D011817:Rabbits; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
chemical_list: D004655:Emulsions; D001566:Benzocaine; D007213:Indomethacin
keywords: Benzocaine microemulsion; eucalyptus oil; indomethacin transdermal; pinprick assay; topical analgesia